Design, diversity-oriented synthesis and structure activity relationship studies of quinolinyl heterocycles as antimycobacterial agents

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• 作者：Venkatesham Rachakonda ; Manjula Alla ; Sudha Sravanti Kotipalli ; Ramesh Ummani
• 关键词：Tuberculosis ; Cytotoxicity ; Antimycobacterial ; Diversity oriented synthesis ; Bis heterocycles ; 3-Acyl/carboxylate-quinoline
• 刊名：European Journal of Medicinal Chemistry
• 出版年：December, 2013
• 年：2013
• 卷：70
• 期：Complete
• 页码：536-547
• 全文大小：448 K

文摘

The current study reports design and diversity oriented synthesis of novel bis heterocycles with a common 2-methyl, C-4 unsubstituted quinoline moiety as the central key heterocycle. Employing reagent based skeletal diversity approach; a facile synthesis of bis heterocycles with different heterocyclic rings at C-3 position of the quinoline moiety has been accomplished. A broad range of heterocyclic frameworks thus obtained were evaluated for their antimycobacterial activity. The active scaffolds were further explored by a parallel library generation in order to establish SAR. Further, low cytotoxicity against A549 cell line enhances the potential of the synthesized molecules as promising antimycobacterial agents.